1,2-diazoles Patents (Class 514/403)
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Publication number: 20110281868Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein A1, A2, A3 and L are defined in the description. The present invention relates also to methods of making said compounds, and compositions containing said compounds which are useful for inhibiting kinases such as aurora and KDR.Type: ApplicationFiled: May 12, 2011Publication date: November 17, 2011Applicant: ABBOTT LABORATORIESInventors: Michael R. Michaelides, James H. Holms, Douglas H. Steinman
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Publication number: 20110275616Abstract: Methods of utilizing an opioid agonist in a mammalian subject in a manner that inhibits peripheral effects of the opioid agonist are described. The methods comprise administering the opioid agonist in an amount sufficient to confer analgesia the subject and co-administering a neutral opioid antagonist or pharmaceutically acceptable isomorph or pharmaceutically acceptable salt thereof in an amount sufficient to substantially inhibit peripheral effects and insufficient to block substantial central effects of the opioid agonist in the subject.Type: ApplicationFiled: July 18, 2011Publication date: November 10, 2011Applicant: AIKO BIOTECHNOLOGYInventors: Wolfgang Sadée, Edward Bilsky, Janet Yancey-Wrona
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Publication number: 20110263662Abstract: The invention relates to 1,2-diamido-ethylene derivatives of the formula (I) wherein R1, R2, R3, and A are as described in the description and their use as medicaments, especially as orexin receptor antagonists.Type: ApplicationFiled: August 14, 2008Publication date: October 27, 2011Inventors: Hamed Aissaoui, Christoph Boss, Markus Gude, Ralf Koberstein, Thierry Sifferlen
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Publication number: 20110257178Abstract: The present invention provides novel pyrazolines that are useful as cannabinoid receptor blockers and pharmaceutical compositions thereof and methods of using the same for treating obesity, diabetes, inflammatory disorders, cardiometabolic disorders, hepatic disorders, and/or cancers.Type: ApplicationFiled: October 7, 2010Publication date: October 20, 2011Applicant: JENRIN DISCOVERYInventors: John F. McElroy, Robert J. Chorvat
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Publication number: 20110245204Abstract: The present invention provides sphingosine-1-phosphate analogs that are potent, and selective agonists at one or more S1P receptors, specifically the S1P1 receptor type. The compounds invention include compounds having a phosphate moiety as well as compounds with hydrolysis-resistant phosphate surrogates such as phosphonates, alpha-substituted phosphonates, and phosphothionates.Type: ApplicationFiled: July 12, 2010Publication date: October 6, 2011Inventors: Kevin R. Lynch, Timothy L. MacDonald
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Patent number: 8030304Abstract: The present invention relates to compounds of Formula (I), pharmaceutical compositions thereof, and use thereof as corticotropin releasing factor 1 (CRF1) receptor antagonists in the treatment of psychiatric and neuroendocrine disorders, neurological diseases, and metabolic syndrome.Type: GrantFiled: September 17, 2007Date of Patent: October 4, 2011Assignee: Eli Lilly and CompanyInventors: Zhaogen Chen, Chafiq Hamdouchi Hamdouchi, Erik James Hembre, Philip Arthur Hipskind, Jason Kenneth Myers, Takako Takakuwa, James Lee Toth
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Patent number: 8030323Abstract: A compound of formula (I) or pharmaceutically acceptable salts and/or solvates or hydrates thereof. A process for preparing the compound, a pharmaceutical composition comprising the compound and an application for resisting cannabinoid CB1 receptor are provided.Type: GrantFiled: January 10, 2007Date of Patent: October 4, 2011Assignee: Beijing Molecule Science and Technology Co., Ltd.Inventors: Song Li, Mengjia Liu, Zhibing Zheng
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Patent number: 8030340Abstract: Compounds of formula (I): or a pharmaceutically acceptable salt thereof, compositions comprising them, processes for preparing them and their use in medical therapy (for example modulating the glucocorticoid receptor in a warm blooded animal).Type: GrantFiled: November 21, 2007Date of Patent: October 4, 2011Assignees: AstraZeneca AB, Bayer Schering Pharma AktiengesellschaftInventors: Markus Berger, Lena Bergstrom, Jan Dahmen, Anders Eriksson, Balint Gabos, Martin Hemmerling, Krister Henriksson, Svetlana Ivanova, Matti Lepisto, Stinabritt Nilsson, Camilla Taflin, Hartmut Rehwinkel, Darren McKerrecher
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Publication number: 20110230488Abstract: The present invention relates to the synthesis of a series of ionone and curcumin derivatives as multi-targeting agents effective against both hormone-sensitive and hormone-independent cancers. In particular, the present invention is directed to a distinct class of bifunctional antiandrogens, which inhibit both AR and IKBkinases (IKK). A series of ionone-based chalcones were synthesised and their in vitro cytotoxicity against prostate cancer cell lines were demonstrated. A series of derivatives formed by reacting ionone-based chalcones and hydrazines demonstrate substantial antiproliferative activities in prostate cancer, breast cancer and lung cancer cell lines.Type: ApplicationFiled: November 25, 2009Publication date: September 22, 2011Applicant: TRT PHARMA INC.Inventors: Jian Hui Wu, Gerald Batist, Jinming Zhou, Guoyan Geng, Rongtuan Lin
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Patent number: 8017558Abstract: Novel carboxamides of the formula (I) The present application is further directed toward a plurality of processes for preparing these compounds and their use for controlling unwanted microorganisms, and also novel intermediates and their preparation.Type: GrantFiled: December 5, 2006Date of Patent: September 13, 2011Assignee: Bayer Cropscience AGInventors: Ralf Dunkel, Hans-Ludwig Elbe, Jörg Nico Greul, Herbert Gayer, Bernd-Wieland Krüger, Arnd Voerste, Ulrike Wachendorff-Neumann, Peter Dahmen
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Patent number: 8017635Abstract: Certain novel phenylalkyl substituted azole derivatives have unexpected insecticidal activity. These compounds are represented by formula I: where A, B, D, E, G, a, b, c, d, and R through R11, inclusively, are folly described herein. In addition, compositions comprising an insecticidally effective amount of at least one compound of formula I, and optionally, an effective amount of at least one of a second compound, with at least one insecticidally compatible carrier are also disclosed; along with methods of controlling insects comprising applying said compositions to a locus where insects are present or are expected to be present.Type: GrantFiled: May 24, 2006Date of Patent: September 13, 2011Assignee: FMC CorporationInventors: John W. Lyga, Frank Zawacki, Larry Y. Zhang
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Patent number: 8012499Abstract: Disclosed are compounds of Formula (1), including all geometric and stereoisomers, N-oxides, and salts thereof, wherein R3 is —C(?B)C(?O)L or —C(R11R12)C(?O)L; R4 is, inter alia, H, C1-C4 alkyl or C2-C6 alkoxycarbonyl; or R3 and R4 are taken together as —C(?O)C(?O)—, —C(?NR13)C(?O)— or —C(R11R12)C(?O)—. B is O, NR13, NOR13 Or NNR14 R15; L is OH or NR14 R15; and X, R1, R2, R11, R12, R13, R14, R15 and J are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula (1) and methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound or a composition of the invention.Type: GrantFiled: August 22, 2006Date of Patent: September 6, 2011Assignee: E.I. du Pont de Nemours and CompanyInventors: Bruce Lawrence Finkelstein, Stephen Frederick McCann
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Patent number: 8008290Abstract: A first aspect of the invention relates to a compound of formula (I), or a pharmaceutically acceptable salt, hydrate, complex or pro-drug thereof, wherein: R3 is selected from cyclopentyl and cyclohexyl; R9 is a substituted 5 or 6-membered aryl or heteroaryl group or a 6,5- or 6,6-fused biaryl or heterobiaryl group. Compounds of formula (I) exhibit surprisingly high dual efficacies for human cathepsin S and K and are useful for the treatment of rheumatoid arthritis, osteoarthritis, chronic obstructive pulmonary disease (COPD), atherosclerosis, cardiovascular diseases which exhibit significant damage and remodeling of extracellular matrix (ECM) and chronic pain.Type: GrantFiled: August 9, 2010Date of Patent: August 30, 2011Assignee: Amura Therapeutics LimitedInventors: Martin Quibell, John P. Watts, Nicholas S. Flinn
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Patent number: 8008327Abstract: Disclosed indazoles compounds that are useful as antagonists of CCR1 activity and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of CCR1 including autoimmune diseases, such as rheumatoid arthritis and multiple sclerosis. Also disclosed are pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.Type: GrantFiled: April 23, 2009Date of Patent: August 30, 2011Assignee: Boehringer Ingelheim International GmbHInventors: Darren DiSalvo, Daniel Kuzmich, Can Mao, Hossein Razavi, Christopher Ronald Sarko, Alan David Swinamer, David Smith Thomson, Qiang Zhang
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Patent number: 7998996Abstract: The present invention relates to substituted pyrazoline compounds, methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans and animal.Type: GrantFiled: February 14, 2005Date of Patent: August 16, 2011Assignee: Laboratorios del Dr. Esteve S.A.Inventors: Rosa Cuberes Altisen, Bonifacio Gutierrez Silva, Jordi Frigola-Constansa
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Publication number: 20110195977Abstract: Acrylamido derivatives useful as therapeutic agents, particularly for the prevention and/or treatment of diseases and conditions associated with the activity of the mitochondrial permeability transition pore (MPTP), such as the diseases characterized by ischemia/reperfusion, oxidative or degenerative tissue damage, are herein described. These compounds belong to the structural formula (I) wherein R, R?, R?, W and a are as defined in the specification. The invention also relates to the preparation of these compounds, as well as to pharmaceutical compositions comprising them.Type: ApplicationFiled: September 23, 2009Publication date: August 11, 2011Inventors: Daniele Fancelli, Varasi Mario, Simon Plyte, Marco Ballarini, Anna Cappa, Giacomo Carenzi, Saverio Minucci, Gilles Pain, Manuela Villa
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Patent number: 7994200Abstract: The present invention relates to Cycloalkane-substituted substituted pyrazoline compounds of formula (I), methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans and animals.Type: GrantFiled: July 17, 2006Date of Patent: August 9, 2011Assignee: Laboratorios del Dr. Esteve, S.A.Inventors: Antonio Torrens Jover, Susana Yenes Minguez
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Patent number: 7994207Abstract: The present invention relates to a process for preparing fluoromethyl-substituted heterocyclic compounds of the general formula (I) in which R1 is H or F; R2 is an -[A-O]m—R3 group in which A is C2-C4-alkanediyl, R3 is C1-C4-alkyl and m is 1 or 2; by converting the corresponding chloromethyl-substituted compounds (II) in the presence of fluorinating agents, to processes for preparing the chloromethyl-substituted compounds (II), to processes for preparing amides of the general formula (IV) and to compounds of the general formulae (I) and (II).Type: GrantFiled: December 20, 2007Date of Patent: August 9, 2011Assignee: BASF SEInventors: Thomas Zierke, Michael Rack
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Publication number: 20110190257Abstract: The invention relates to bicyclic heterocycles of formulae I and II with anti-cancer and/or anti-inflammatory activity and more specifically with MEK kinase inhibitory activity. The invention provides compositions and methods useful for inhibiting abnormal cell growth, treating a hyperproliferative disorder, or treating an inflammatory disease in a mammal. The invention also relates to methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.Type: ApplicationFiled: July 1, 2009Publication date: August 4, 2011Applicant: Genetech, Inc.Inventors: Robert Andrew Heald, Philip Jackson, Joseph P. Lyssikatos, Stephen Price, Pascal Pierre Alexandre Savy
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Patent number: 7989475Abstract: The present invention relates to substituted pyrazoles, compositions containing such compounds and methods of treatment The compounds are glucagon receptor antagonists and thus are useful for treating, preventing or delaying the onset of type 2 diabetes mellitus.Type: GrantFiled: March 19, 2009Date of Patent: August 2, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Emma Parmee, Subharekha Raghavan, Teresa Beeson, Dong-Ming Shen
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Publication number: 20110183939Abstract: The present invention provides a novel P2X3 and/or P2X2/3 receptor antagonist. A compound represented by the formula (I); wherein Z1 is optionally protected hydroxy, etc.; Z2 is —C(?O)—, etc.; Z3a and Z3b are taken together ?O or ?S; t is an integer of 0 to 4; R4a and R4b are each independently, hydrogen or substituted or unsubstituted lower alkyl, etc.; m and n are each independently an integer of 0 to 2; k is an integer of 0 or 1; Ring A is an aromatic carbocyclic ring or a heterocyclic ring, etc.; B is aromatic carbocyclic ring-diyl or heterocyclic ring-diyl, etc.; R1a and R1b are each independently halogen, hydroxy, substituted or unsubstituted lower alkyl, etc.; R2 is substituted or unsubstituted alkyl, etc.; R3 is substituted or unsubstituted alkyl, substituted or unsubstituted aryl or a substituted or unsubstituted heterocyclic group, etc.; or its pharmaceutically acceptable salt, or a solvate thereof is provided.Type: ApplicationFiled: September 24, 2009Publication date: July 28, 2011Applicant: SHIONOGI & CO., LTD.Inventors: Hiroyuki Kai, Yoshiyuki Taoda, Takeshi Endoh, Tohru Horiguchi, Kentaro Asahi, Hiroyuki Tobinaga
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Publication number: 20110183952Abstract: The present invention encompasses compounds of general formula (1), wherein the groups R1 to R3 and L are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and their use for preparing a medicament having the above-mentioned properties.Type: ApplicationFiled: July 1, 2008Publication date: July 28, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Ioannis Sapountzis, Peter Ettmayer, Christian Klein, Andreas Mantoulidis, Steffen Steurer, Irene Waizenegger
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Publication number: 20110183977Abstract: Disclosed are compounds and pharmaceutically acceptable salts of Formula I wherein R1, R2, R3, R4, R5, R6, R7, n, Q1, Q2, Q3, Y, and X1-X4 are as defined herein. Compounds of Formula I are useful in the treatment of diseases and/or conditions related to cell proliferation, such as cancer, inflammation, arthritis, angiogenesis, or the like. Also disclosed are pharmaceutical compositions comprising compounds of the invention and methods of treating the aforementioned conditions using such compounds.Type: ApplicationFiled: April 7, 2011Publication date: July 28, 2011Applicant: Serenex, Inc.Inventors: Kenneth He Huang, Jeron Eaves, Gunnar J. Hanson, James Veal, Thomas Barta, Lifeng Geng, Lindsay Hinkley
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Patent number: 7977366Abstract: The present invention relates to a method of treating an inflammatory disorder in a subject with an effective amount of compound having the general formula (I) as described in the present application, under conditions effective to treat the inflammatory disorder. The present invention also relates to a method of inhibiting respiratory burst in neutrophils without inhibiting degranulation in or bacterial killing by the neutrophils by contacting neutrophils with the compounds described above.Type: GrantFiled: October 14, 2004Date of Patent: July 12, 2011Assignee: Cornell Research Foundation, Inc.Inventors: Hyunsil Han, Gang Lin, Carl Nathan
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Patent number: 7977364Abstract: The present invention relates to compounds of formula (I): in which R1, R2, R3, X, Y and A are as defined in the specification. The compounds are modulators of the estrogen receptors.Type: GrantFiled: October 14, 2005Date of Patent: July 12, 2011Assignee: Laboratoire ThermamexInventors: Benoit Rondot, Jean Lafay, Paule Bonnet, Thierry Clerc, Igor Duc, Eric Duranti, Francois Puccio, Jacqueline Shields, Christian Blot, Philippe Maillos
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Patent number: 7973061Abstract: The present invention relates to compounds of the Formula I, wherein L, X, Y, Z, R1, R2, R3 and R4 are defined herein. The invention also provides methods of using the compounds for inhibition of kinases, more specifically ALK kinases. The invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. Compounds of the invention inhibit, regulate and/or modulate kinase receptor signal transduction pathways related to the changes in cellular activities as mentioned above, and the invention includes compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions; (Formula I).Type: GrantFiled: March 31, 2005Date of Patent: July 5, 2011Assignee: Exelixis, Inc.Inventors: James William Leahy, Gary Lee Lewis, John M. Nuss, Brain Hugh Ridgway, Joan C. Sangalang
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Patent number: 7968582Abstract: The present invention relates to substituted pyrazoline compounds, methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans and animals.Type: GrantFiled: July 14, 2006Date of Patent: June 28, 2011Assignee: Laborotorios Del Dr. Esteve, S.A.Inventor: Rosa Cuberes
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Patent number: 7968584Abstract: This invention relates to a range of 1-aryl-4-cyclopropylpyrazoles in which the cyclopropyl ring is substituted at the angular position, and pharmaceutically acceptable salts and solvates thereof, to compositions comprising such compounds, processes to their synthesis and their use as parasiticides.Type: GrantFiled: March 19, 2009Date of Patent: June 28, 2011Assignees: Pfizer Inc., Pfizer Products Inc.Inventors: Denis Billen, Jessica Boyle, Douglas James Critcher, David Morris Gethin, Kim Thomas Hall, Graham Michael Kyne
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Patent number: 7968579Abstract: Disclosed herein are antifungal triazole derivatives or pharmaceutically acceptable salts thereof, a preparation method thereof, and a pharmaceutical composition comprising the same. The triazole derivatives of Chemical Formula 1 or pharmaceutically acceptable salts thereof according to the present invention have excellent inhibitory activity against a broad spectrum of fungi, in addition to being safe to the body, and thus are very useful in the treatment and prevention of fungal infection.Type: GrantFiled: October 31, 2006Date of Patent: June 28, 2011Assignee: Daewoong Pharmaceutical Co., Ltd.Inventors: Joon Seok Park, Kyung A Yu, Sun Young Kim, Yeon Jung Song, Kang-Pil Kim, Yun Soo Yoon, Mi Ryeong Han
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Publication number: 20110152250Abstract: Compounds that are antagonists of the VR1 receptor, having formula (I) or a pharmaceutically acceptable salt, prodrug, or salt of a prodrug thereof, wherein A1, A2, A3, A4, R7, R8, R9, X, Y, Z, L, n, and m, are as defined herein, and are useful in disorders prevented or ameliorated by inhibiting the VR1 receptor.Type: ApplicationFiled: September 3, 2010Publication date: June 23, 2011Applicant: ABBOTT LABORATORIESInventors: Arthur Gomtsyan, Erol K. Bayburt, Robert G. Schmidt, JR., Chih-Hung Lee, Brian S. Brown, Tammie K. Jinkerson, John R. Koenig, Jerome F. Daanen, Steven P. Latshaw
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Patent number: 7960588Abstract: Sphingosine-1-phosphate analogs that are potent, and selective agonists at one or more S1P receptors, specifically the S1P1 receptor type are provided. The disclosed compounds include an optional phosphate moiety as well as compounds with hydrolysis-resistant phosphate surrogates such as phosphonates, alpha-substituted phosphonates, and phosphothionates.Type: GrantFiled: March 29, 2010Date of Patent: June 14, 2011Assignee: University of Virginia Patent FoundationInventors: Kevin R. Lynch, Timothy L. Macdonald
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Patent number: 7960426Abstract: This invention relates to a combination product comprising a compound of formula I wherein X, R1, R2, R3, R4, R5, R6, R7 and R9 are as described herein, and one or more further biologically active compounds as described herein, particularly anti-parasitic agents.Type: GrantFiled: February 3, 2009Date of Patent: June 14, 2011Assignee: Pfizer LimitedInventors: Denis Billen, Nathan Anthony Logan Chubb, David Morris Gethin, Kim Thomas Hall, Lee Richard Roberts, Nigel Derek Arthur Walshe
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Patent number: 7956060Abstract: The present invention provides an antitumor agent and the like, which comprises as an active ingredient, a pyrimidine derivative represented by Formula (I): [wherein —X—Y—Z— represents —O—CR3?N— (wherein R3 represents a hydrogen atom, a substituted or unsubstituted aromatic heterocyclic group and the like) and the like, R1 represents —NR10R11 (wherein R10 and R11 may be the same or different, and each represents a hydrogen atom, substituted or unsubstituted lower alkyl and the like) and the like, R2 represents —NR13R14 (wherein R13 and R14 may be the same or different, and each represents a hydrogen atom, substituted or unsubstituted lower alkyl and the like)] or a pharmaceutically acceptable salt thereof.Type: GrantFiled: March 30, 2005Date of Patent: June 7, 2011Assignee: Kyowa Hakko Kirin Co., Ltd.Inventors: Hitoshi Arai, Tsutomu Matsumura, Syoichi Isami, Hiroshi Ishida, Koji Hagihara, Hiroshi Umehara, Yoshinori Yamashita, Nana Oiwa, Yukimasa Shiotsu, Tomoki Naoe, Hitoshi Kiyoi
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Patent number: 7951830Abstract: The invention relates to the use of a compound of Formula (I) or a salt, solvate or prodrug thereof, wherein R1, R2, R3, n and m are as described in the specification, in the preparation of a medicament for the treatment or prevention of a disease condition mediated through glucokinase (GLK), such as type 2 diabetes. The invention also relates to a novel group of compounds of Formula (I) and to methods for preparing compounds of Formula (I).Type: GrantFiled: February 2, 2009Date of Patent: May 31, 2011Assignee: AstraZeneca ABInventors: Scott Boyd, Peter William Rodney Caulkett, Rodney Brian Hargreaves, Suzanne Saxon Bowker, Roger James, Clifford David Jones, Darren McKerrecher, Michael Howard Block, Craig Johnstone
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Publication number: 20110124669Abstract: The present invention provides compounds having formula (I): and pharmaceutically acceptable derivatives thereof, wherein R1-R4, n, p, A, B, D, E, L and AR1 are as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of disorders mediated by the CD11/CD18 family of cellular adhesion molecules (e.g., LFA-1).Type: ApplicationFiled: February 4, 2011Publication date: May 26, 2011Applicant: SARcode CorporationInventors: Wang Shen, Kenneth Barr, Johan D. Oslob, Min Zhong
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Patent number: 7943653Abstract: This invention is directed to a cannabinoid modulator compound of formula (I): or a form thereof, and methods for use in treating, ameliorating or preventing a cannabinoid receptor mediated syndrome, disorder or disease.Type: GrantFiled: August 11, 2008Date of Patent: May 17, 2011Assignee: Janssen Pharmaceutica N.V.Inventors: Mingde Xia, Meng Pan, Michael P. Wachter
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Patent number: 7943652Abstract: The present teachings relate to compounds of Formula I: and pharmaceutically acceptable salts, hydrates, esters, and prodrugs thereof, wherein R1, R2, R3, Y, Z, and are as defined herein. The present teachings also provide methods of preparing compounds of Formula I and methods of using compounds of Formula I in treating, inhibiting, or preventing pathologic conditions or disorders mediated wholly or in part by deacetylases.Type: GrantFiled: March 26, 2009Date of Patent: May 17, 2011Assignee: Novartis AGInventors: Michael D. Shultz, Christine Hiu-Tung Chen, Young Shin Cho, Lei Jiang, Jianmei Fan, Gang Liu, Dyuti Majumdar, Jianke Li
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Patent number: 7943651Abstract: The present invention provides compounds of formula (I): pharmaceutical compositions comprising the compounds and the use of the compounds for the manufacture of a medicament, particularly for the treatment of inflammation and/or allergic conditions.Type: GrantFiled: April 18, 2007Date of Patent: May 17, 2011Assignee: Glaxo Group LimitedInventors: Keith Biggadike, Anthony William James Cooper, David House, Iain McFarlane McLay
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Patent number: 7939520Abstract: The present invention provides a compound of formula I and the use thereof in the therapeutic treatment of disorders related to or affected by the 5-HT6 receptor.Type: GrantFiled: May 13, 2008Date of Patent: May 10, 2011Assignee: Wyeth LLCInventors: Simon Nicolas Haydar, Patrick Andrae
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Patent number: 7935720Abstract: In the case of using 3-[3-amino-4-(indan-2-yloxy)-5-(1-methyl-1H-indazol-5-yl)phenyl]propionic acid, methyl 3-[4-(indan-2-yloxy)-3-(1-methyl-1H-indazol-5-yl)-5-nitrophenyl]propionate, or methyl 3-[3-amino-4-(indan-2-yloxy)-5-(1-methyl-1H-indazol-5-yl)phenyl]propionate as a medicine, more preferable aspects or improved methods are provided. Crystals of any compound among 3-[3-amino-4-(indan-2-yloxy)-5-(1-methyl-1H-indazol-5-yl)phenyl]propionic acid, methyl 3-[4-(indan-2-yloxy)-3-(1-methyl-1H-indazol-5-yl)-5-nitrophenyl]propionate, and methyl 3-[3-amino-4-(indan-2-yloxy)-5-(1-methyl-1H-indazol-5-yl)phenyl]propionate, and methods of producing the same are provided.Type: GrantFiled: October 5, 2010Date of Patent: May 3, 2011Assignee: Asahi Kasei Pharma CorporationInventor: Motoshi Shoda
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Patent number: 7928135Abstract: Disclosed are compounds and pharmaceutically acceptable salts of Formula I wherein R1, R2, R3, R4, R5, R6, R7, n, Q1, Q2, Q3, Y, and X1-X4 are as defined herein. Compounds of Formula I are useful in the treatment of diseases and/or conditions related to cell proliferation, such as cancer, inflammation, arthritis, angiogenesis, or the like. Also disclosed are pharmaceutical compositions comprising compounds of the invention and methods of treating the aforementioned conditions using such compounds.Type: GrantFiled: October 19, 2010Date of Patent: April 19, 2011Assignee: Serenex, Inc.Inventors: Kenneth He Huang, Jeron Eaves, Gunnar Hanson, James Veal, Thomas Barta, Lifeng Geng, Lindsay Hinkley
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Patent number: 7927613Abstract: A pharmaceutical composition comprising a co-crystal of an API and a co-crystal former; wherein the API has at least one functional group selected from ether, thioether, alcohol, thiol, aldehyde, ketone, thioketone, nitrate ester, phosphate ester, thiophosphate ester, ester, thioester, sulfate ester, carboxylic acid, phosphonic acid, phosphinic acid, sulfonic acid, amide, primary amine, secondary amine, ammonia, tertiary amine, sp2 amine, thiocyanate, cyanamide, oxime, nitrile diazo, organohalide, nitro, s-heterocyclic ring, thiophene, n-heterocyclic ring, pyrrole, o-heterocyclic ring, furan, epoxide, peroxide, hydroxamic acid, imidazole, pyridine and the co-crystal former has at least one functional group selected from amine, amide, pyridine, imidazole, indole, pyrrolidine, carbonyl, carboxyl, hydroxyl, phenol, sulfone, sulfonyl, mercapto and methyl thio, such that the API and co-crystal former are capable of co-crystallizing from a solution phase under crystallization conditions.Type: GrantFiled: September 11, 2003Date of Patent: April 19, 2011Assignees: University of South Florida, The Regents of the University of Michigan, Transform Pharmaceuticals, Inc.Inventors: Örn Almarsson, Magali Bourghol Hickey, Matthew L. Peterson, Michael J. Zaworotko, Brian Moulton, Nair Rodriguez-Hornedo
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Patent number: 7928134Abstract: The invention is directed to 5-(hetero)aryl-4,5-dihydro-(1H)-pyrazole (pyrazoline) derivatives as cannabinoid CB1 receptor agonists, to pharmaceutical compositions comprising these compounds, to methods for their syntheses, methods for preparing novel intermediates useful for their syntheses, and methods for preparing compositions. The invention also relates to the uses of such compounds and compositions, administered to patients to achieve a therapeutic effect in disorders in which CB1 receptors are involved, or that can be treated via manipulation of those receptors. Compounds of the present invention include compounds of formula (I): wherein the substituents have the definitions given in the specification.Type: GrantFiled: September 19, 2008Date of Patent: April 19, 2011Assignee: Solvay Pharmaceuticals B.V.Inventors: Josephus H. M. Lange, Hicham Zilaout, Bernard J. Van Vliet
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Patent number: 7923465Abstract: The present invention relates to novel cannabinoid receptor modulators, in particular cannabinoid 1 (CB1) or cannabinoid 2 (CB2) receptor modulators, and uses thereof for treating diseases, conditions and/or disorders modulated by a cannabinoid receptor (such as pain, neurodegenerative disorders, eating disorders, weight loss or control, and obesity).Type: GrantFiled: June 1, 2006Date of Patent: April 12, 2011Assignee: Glenmark Pharmaceuticals S.A.Inventors: Meyyappan Muthuppalaniappan, Gopalan Balasubramanian, Srinivas Gullapalli, Neelima Khairatkar Joshi, Shridhar Narayanan
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Patent number: 7919517Abstract: The present invention provides a compound represented by Formula (I): [wherein R1 represents CONR1aR1b (wherein R1a and R1b may be the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl, substituted or unsubstituted ararkyl or a substituted or unsubstituted heterocyclic group, or R1a and R1b are combined together with the adjacent nitrogen atom thereto to form a substituted or unsubstituted heterocyclic group) or the like, R2 represents a hydrogen atom, CONR2aR2b (wherein R2a and R2b may be the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl, substituted or unsubstituted ararkyl or a substituted or unsubstituted heterocyclic group, or R2a and R2b are combined together with the adjacent nitrogen atom thereto to form a substituted or unsubstituted heterocyclic group), NR2cR2d (wherein R2c and R2d may be the same or different and each represents aType: GrantFiled: November 21, 2008Date of Patent: April 5, 2011Assignee: Kyowa Hakko Kirin Co., Ltd.Inventors: Yoshihisa Ohta, Fumihiko Kanai, Shinji Nara, Yutaka Kanda, Hiroshi Umehara, Yukimasa Shiotsu, Tomoki Naoe, Hitoshi Kiyoi, Keiko Kawashima, Hiromi Ando, Motoki Miyama
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Publication number: 20110077250Abstract: The invention relates to compositions and methods for inhibiting RNA binding proteins (e.g., MEX-3, MEX-5 and POS-1), as well as methods for treating and preventing disorders associated with parasitic infections and inflammatory disorders.Type: ApplicationFiled: June 25, 2010Publication date: March 31, 2011Inventor: Sean RYDER
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Patent number: 7915250Abstract: Disclosed are compounds of Formula (I) and pharmaceutically acceptable salts and solvates thereof. Such compounds are MEK inhibitors and are useful in the treatment of proliferative diseases, such as cancer. Also disclosed are pharmaceutical compositions containing such compounds as well as methods of using the compounds and compositions of the invention in the treatment of cancer.Type: GrantFiled: May 5, 2010Date of Patent: March 29, 2011Assignee: Exelixis, Inc.Inventors: Naing Aay, Neel Kumar Anand, Charles M. Blazey, Owen Joseph Bowles, Joerg Bussenius, Simona Costanzo, Jeffry Kimo Curtis, Steven Charles DeFina, Larisa Dubenko, Anagha Abhijit Joshi, Abigail R. Kennedy, Angie Inyoung Kim, Elena S. Koltun, Jean-Claire Limun Manalo, Csaba J. Peto, Kenneth D. Rice, Tsze H. Tsang
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Publication number: 20110071146Abstract: To provide a novel and excellent method for treating and/or preventing prostatic cancer, benign prostatic hyperplasia, acne, seborrhea, hirsutism, baldness, alopecia, precocious puberty, adrenal hypertrophy, polycystic ovary syndrome, breast cancer, lung cancer, endometriosis, leiomyoma and the like based on selective inhibitory activity against 17?HSD type 5. It was found that an N-sulfonylindole derivative, where the indole ring is substituted by a carboxy group, a carboxy-substituted lower alkyl group or a carboxy-substituted lower alkenyl group at its carbon atom, has potent selective inhibitory activity against 17?HSD type 5 and may become a therapeutic agent and/or preventive agent for benign prostatic hyperplasia, prostatic cancer and the like without accompanying adverse drug reactions due to a decrease in testosterone, and the present invention has thus been completed.Type: ApplicationFiled: November 10, 2010Publication date: March 24, 2011Inventors: Tatsuya Niimi, Akio Kamikawa, Yasushi Amano, Tomohiko Yamaguchi, Kenichi Suzumura, Kentaro Enjo, Takashi Furutani, Akio Kakefuda, Yutaka Kondoh, Masaaki Hirano
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Patent number: 7902248Abstract: Disclosed herein are pyrazole glucokinase activators of the formula (I): that are useful for the treatment of metabolic diseases and disorders.Type: GrantFiled: December 6, 2007Date of Patent: March 8, 2011Assignee: Hoffmann-La Roche Inc.Inventors: Steven Joseph Berthel, Robert Francis Kester, Douglas Eric Murphy, Thomas Jay Prins, Frank Ruebsam, Chinh Viet Tran, Dionisios Vourloumis
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Patent number: 7901701Abstract: Disclosed are compositions and methods related to powder and granular emulsifiable concentrate pesticide formulations. As disclosed, emulsions from non-aqueous based liquid or solvent soluble pesticide actives may be prepared using a high purity, high molecular weight sulfonated lignin as the emulsion stabilizer. The resulting emulsions may then be dried to obtain a powder or granular emulsion concentrate where the high molecular weight sulfonated lignin acts as a solid matrix for the pesticide active. The powder or granular emulsifiable concentrate formulations thus formed have high loading rates, good storage properties and are easily reconstituted when added to water.Type: GrantFiled: October 29, 2007Date of Patent: March 8, 2011Assignee: Lignotech USA, Inc.Inventors: Thomas S. Winowiski, Stuart E. Lebo, Scott E. Davis, Stig Are Gundersen